局所麻酔剤の研究 (第6報)

プロカインモノ置換体の薬効に就いて

抄録

In order to make systematic observations on the capacity of the auxiliary atomic groups with local anesthetic properties, 22 kinds of ortho- or meta-substituted derivatives of procaine were prepared, 11 of which being new compounds. Tests of surface filtrating anesthetic action and toxicity revealed that the substituents in general increased the effect of procaine without giving a large effect on the toxicity. Electron-donating radicals were more effective in the ortho-position than in the meta, while electron-attracting groups seemed to be more effective in the meta-position. Of the compounds prepared, those introduced with thiomethyl or thioethyl groups were the most effective, showing 1.5 times the surface anesthetic action than cocaine. Alkoxyl and halogen substituents followed the above in efficacy.